Allosteric potentiator at the adenosine A1
receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t½
of dissociation from, the receptor. Also inhibits basal and forskolin-stimulated adenylyl cyclase (AC) activity in A1
receptors expressed in CHO cells, possibly via direct potentiation of constitutive receptor activity or by direct inhibition of AC. Active in vivo
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Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes.
Bruns et al.
Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor.
Kollias-Baker et al.
PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs.
Mizumura et al.
Adenosine A1 receptor-dependent and -independent effects of the allosteric enhancer PD 81,723.
Musser et al.